Structural Insights into Endothelin Receptor Signaling

Endothelins and their receptors, ETA and ETB, modulate vital cellular processes, including growth, survival, invasion, and angiogenesis, through multiple G proteins. This review highlights the structural determinations of these receptors by X-ray crystallography and cryo-electron microscopy, and the...

Full description

Saved in:
Bibliographic Details
Published in:Journal of biochemistry (Tokyo) Vol. 174; no. 4; p. 317
Main Authors: Shihoya, Wataru, Sano, Fumiya K, Nureki, Osamu
Format: Journal Article
Language:English
Published: England 01.10.2023
Subjects:
SBDD
Endothelin
Vascular system
Structural biology
G-protein-coupled receptor
ISSN:1756-2651, 1756-2651
Online Access:Get more information
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Endothelins and their receptors, ETA and ETB, modulate vital cellular processes, including growth, survival, invasion, and angiogenesis, through multiple G proteins. This review highlights the structural determinations of these receptors by X-ray crystallography and cryo-electron microscopy, and their activation mechanisms by endothelins. Explorations of the conformational changes upon receptor activation have provided insights into the unique G-protein coupling feature of the endothelin receptors. The review further delves into the binding modes of the clinical antagonist and the inverse agonists. These findings significantly contribute to understanding the mechanism of G-protein activation and have potential implications for drug development, particularly in the context of vasodilatory antagonists and agonists targeting the endothelin receptors.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
content type line 23
ObjectType-Review-1
ISSN:1756-2651
1756-2651
DOI:10.1093/jb/mvad055